675599-62-9

PG-01037 is a selective dopamine D₃ receptor antagonist (K_is = 0.7, 93, and 375 nM for HEK293 cells expressing human D₃, D₂, and D₄ receptors, respectively). It inhibits quinpirole-induced stimulation of mitogenesis in CHO cells expressing human dopamine D₃ receptors (EC₅₀ = 3 nM). PG-01037 (32 mg/kg) reduces progressive-ratio methamphetamine self-administration in rats allowed extended access. It reduces loss of dopaminergic neurons in the substantia nigra pars compacta and improves motor performance in the coat-hanger test in a mouse model of Parkinson''s disease induced by MPTP.

PG01037 dihydrochloride is a selective D3DR antagonist.

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[1] PETER GRUNDT. Novel Heterocyclic Trans Olefin Analogues of N-{4-[4-(2,3-Dichlorophenyl)piperazin-1-yl]butyl}arylcarboxamides as Selective Probes with High Affinity for the Dopamine D3 Receptor[J]. Journal of Medicinal Chemistry, 2005, 48 3: 839-848. DOI: 10.1021/jm049465g
[2] LAURA ORIO. PRECLINICAL STUDY: FULL ARTICLE: The dopamine D3 receptor partial agonist CJB090 and antagonist PG01037 decrease progressive ratio responding for methamphetamine in rats with extended-access[J]. Addiction Biology, 2010, 15 3: 312-323. DOI: 10.1111/j.1369-1600.2010.00211.x
[3] DANIELA ELGUETA . Pharmacologic antagonism of dopamine receptor D3 attenuates neurodegeneration and motor impairment in a mouse model of Parkinson’s disease[J]. Neuropharmacology, 2017, 113: Pages 110-123. DOI: 10.1016/j.neuropharm.2016.09.028